N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor

Jalaj Arora; Michel Bordeleau; Laurence Dube; Keith Jarvie; Lucy Mazzocco; Jack Peragine; Ashok Tehim; Ian Egle

doi:10.1016/j.bmcl.2005.08.051

N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5253-6. doi: 10.1016/j.bmcl.2005.08.051. Epub 2005 Sep 15.

Authors

Jalaj Arora¹, Michel Bordeleau, Laurence Dube, Keith Jarvie, Lucy Mazzocco, Jack Peragine, Ashok Tehim, Ian Egle

Affiliation

¹ NPS Pharmaceuticals, 6850 Goreway Dr., Mississauga, Ont., Canada L4V 1V7.

PMID: 16168646
DOI: 10.1016/j.bmcl.2005.08.051

Abstract

A series of N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides 8 has been prepared and found to bind with high affinity to the human D(4) (hD(4)) and 5-HT(2A) receptors. Several compounds displayed selectivity for these receptors versus hD(2) and alpha(1) adrenergic receptors of over 500-fold.

MeSH terms

Antipsychotic Agents / chemical synthesis
Antipsychotic Agents / chemistry*
Antipsychotic Agents / pharmacology*
Benzamides / chemical synthesis
Benzamides / chemistry*
Benzamides / pharmacology*
Dopamine / chemistry
Humans
Ligands
Receptors, Dopamine D4 / antagonists & inhibitors*
Serotonin 5-HT2 Receptor Antagonists*

Substances

Antipsychotic Agents
Benzamides
Ligands
Serotonin 5-HT2 Receptor Antagonists
Receptors, Dopamine D4
Dopamine